Artemether | CAS#71963-77-4

MedKoo Cat#: 317250 | Name: Artemether

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Artemether is a natural product which effectively kills both malarial parasites P. falciparum and P. vivax. Artemether is usually used in combination with Lumefantrine for the treatment of malaria. Arthemether also kills trematodes of the species Schistosoma, providing protection against schistosomiasis. Sesquiterpene lactones like artemether, artesunate, and artemisinin have potential applications in certain types of cancer and inflammatory conditions.

Chemical Structure

Artemether

CAS#71963-77-4

Theoretical Analysis

MedKoo Cat#: 317250

Name: Artemether

CAS#: 71963-77-4

Chemical Formula: C16H26O5

Exact Mass: 298.1780

Molecular Weight: 298.37

Elemental Analysis: C, 64.41; H, 8.78; O, 26.81

Price and Availability

Size	Price	Availability
5g	USD 450.00	2 Weeks
10g	USD 750.00	2 Weeks
25g	USD 1,250.00	2 Weeks

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Related CAS #

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Synonym

Artemos; Artenam; Artesaph; Artesian; Dihydroartemisinin Methyl Ether; Falcidol; Gvither; Larither; Malartem; SM 224; β-Artemether; β-Dihydroartemisinin Methyl Ether

IUPAC/Chemical Name

(3R,5aS,6R,8aS,9R,10S,12R,12aR)-decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin

InChi Key

SXYIRMFQILZOAM-HVNFFKDJSA-N

InChi Code

InChI=1S/C16H26O5/c1-9-5-6-12-10(2)13(17-4)18-14-16(12)11(9)7-8-15(3,19-14)20-21-16/h9-14H,5-8H2,1-4H3/t9-,10-,11+,12+,13+,14-,15-,16-/m1/s1

SMILES Code

C[C@@H]1CC[C@H]2[C@H]([C@H](O[C@H]3[C@@]24[C@H]1CC[C@](O3)(OO4)C)OC)C

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Artemether is an antimalarial for the treatment of resistant strains of falciparum malaria.

In vitro activity:

As shown in Figs. 1B and C, ART exhibited strong inhibitory effect on the proliferation of both A549 and NCI-H1299 cells in a dose- and time-dependent manner, among which NCI-H1299 cells were more sensitive to ART (Artemether). P53 gene is null in NCI-H1299 cells, indicating that the inhibitory effect of ART in NSCLC cells was not dependent on p53 status. In addition, this study also tested the cytotoxicity of ART at the same conditions in normal bronchial epithelial cell line BEAS-2B, and observed that normal cells were not sensitive to ART (Figs. 1B, C). These results indicated that ART exhibetes selective sensitivity on NSCLC cells. Forthermore, according to the colony forming assay, this study found that low concentration of ART significantly inhibited the colony formation of detected NSCLC cells (Figs. 1D, E). Taken together, this study reveals that ART not only has inhibitory effect on the proliferation of NSCLC cells but also has a excellent selectivity against NSCLC cells over the normal cells. Reference: Biol Pharm Bull. 2019 Oct 1;42(10):1720-1725. https://pubmed.ncbi.nlm.nih.gov/31378747/

In vivo activity:

At the end of this study, focal segmental glomerulosclerosis (Fig. 2a,j), tubular injury (Fig. 2b,k), and tubulointerstitial fibrosis (Fig. 2c,l) were prominent in AN (Artemether) group mice. Artemether treatment significantly ameliorated these pathological lesions (Fig. 2a–c,j–l). Consistent with the tubular pathological changes, urinary Kim-1 and NGAL levels, which are two tubular injury biomarkers, increased significantly in the AN group and were significantly reduced by artemether (Fig. 2d,e). In addition, the fibrosis-related mRNA (fibronectin: FN, α-smooth muscle actin: α-SMA, collagen: COL I, and COL III) levels also increased significantly in AN group mice and were downregulated by artemether treatment (Fig. 2f–i). Consistent with these molecular and pathological changes, the increased serum creatinine and BUN in AN group were significantly reduced by artemether (Fig. 9a,b). Reference: Sci Rep. 2021; 11: 1266. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7809108/

	Solvent	mg/mL	mM
Solubility
	DMSO	50.0	167.44
	DMF	20.0	67.03
	DMF:PBS (pH 7.2) (1:1)	0.5	1.68
	Ethanol	35.3	118.24

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 298.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Chen J, Huang X, Tao C, Xiao T, Li X, Zeng Q, Ma M, Wu Z. Artemether Attenuates the Progression of Non-small Cell Lung Cancer by Inducing Apoptosis, Cell Cycle Arrest and Promoting Cellular Senescence. Biol Pharm Bull. 2019 Oct 1;42(10):1720-1725. doi: 10.1248/bpb.b19-00391. Epub 2019 Aug 3. PMID: 31378747. 2. Zhao X, Guo X, Yue W, Wang J, Yang J, Chen J. Artemether suppresses cell proliferation and induces apoptosis in diffuse large B cell lymphoma cells. Exp Ther Med. 2017 Nov;14(5):4083-4090. doi: 10.3892/etm.2017.5063. Epub 2017 Aug 29. PMID: 29104626; PMCID: PMC5658687. 3. Han P, Cai Y, Wang Y, Weng W, Chen Y, Wang M, Zhan H, Yu X, Wang T, Shao M, Sun H. Artemether ameliorates kidney injury by restoring redox imbalance and improving mitochondrial function in Adriamycin nephropathy in mice. Sci Rep. 2021 Jan 14;11(1):1266. doi: 10.1038/s41598-020-80298-x. PMID: 33446820; PMCID: PMC7809108. 4. Bai X, Pei R, Lei W, Zhao M, Zhang J, Tian L, Shang J. Antidiabetic Effect of Artemether in Db/Db Mice Involves Regulation of AMPK and PI3K/Akt Pathways. Front Endocrinol (Lausanne). 2020 Sep 25;11:568864. doi: 10.3389/fendo.2020.568864. PMID: 33101203; PMCID: PMC7545317.

In vitro protocol:

In vivo protocol:

1. Han P, Cai Y, Wang Y, Weng W, Chen Y, Wang M, Zhan H, Yu X, Wang T, Shao M, Sun H. Artemether ameliorates kidney injury by restoring redox imbalance and improving mitochondrial function in Adriamycin nephropathy in mice. Sci Rep. 2021 Jan 14;11(1):1266. doi: 10.1038/s41598-020-80298-x. PMID: 33446820; PMCID: PMC7809108. 2. Bai X, Pei R, Lei W, Zhao M, Zhang J, Tian L, Shang J. Antidiabetic Effect of Artemether in Db/Db Mice Involves Regulation of AMPK and PI3K/Akt Pathways. Front Endocrinol (Lausanne). 2020 Sep 25;11:568864. doi: 10.3389/fendo.2020.568864. PMID: 33101203; PMCID: PMC7545317.

1: Swain TR, Raulo A, Mohapatra N, Singha MR. Information Education and Communication can Improve Adherence to Artemether-Lumefantrine Combination in Patients of Uncomplicated Falciparum Malaria. J Clin Diagn Res. 2015 Sep;9(9):FC01-3. doi: 10.7860/JCDR/2015/13196.6544. Epub 2015 Sep 1. PubMed PMID: 26500920. 2: Parikh S, Fehintola F, Huang L, Olson A, Adedeji WA, Darin KM, Morse GD, Murphy RL, Taiwo BO, Akinyinka OO, Adewole IF, Aweeka FT, Scarsi KK. Artemether-lumefantrine exposure in HIV-infected Nigerian subjects on nevirapine-containing antiretroviral therapy. Antimicrob Agents Chemother. 2015 Sep 21. pii: AAC.01153-15. [Epub ahead of print] PubMed PMID: 26392500. 3: WorldWide Antimalarial Resistance Network (WWARN) Lumefantrine PK/PD Study Group. Artemether-lumefantrine treatment of uncomplicated Plasmodium falciparum malaria: a systematic review and meta-analysis of day 7 lumefantrine concentrations and therapeutic response using individual patient data. BMC Med. 2015 Sep 18;13(1):227. doi: 10.1186/s12916-015-0456-7. PubMed PMID: 26381375; PubMed Central PMCID: PMC4574542. 4: Gray AM, Arguin PM, Hamed K. Surveillance for the safety and effectiveness of artemether-lumefantrine in patients with uncomplicated Plasmodium falciparum malaria in the USA: a descriptive analysis. Malar J. 2015 Sep 17;14:349. doi: 10.1186/s12936-015-0881-2. PubMed PMID: 26377423; PubMed Central PMCID: PMC4573675. 5: Yavo W, Konaté A, Kassi FK, Djohan V, Angora EK, Kiki-Barro PC, Vanga-Bosson H, Menan EI. Efficacy and Safety of Artesunate-Amodiaquine versus Artemether-Lumefantrine in the Treatment of Uncomplicated Plasmodium falciparum Malaria in Sentinel Sites across Côte d'Ivoire. Malar Res Treat. 2015;2015:878132. doi: 10.1155/2015/878132. Epub 2015 Aug 12. PubMed PMID: 26347849; PubMed Central PMCID: PMC4549615. 6: Bendel D, Rulisa S, Ansah P, Sirima S. Efficacy of a Novel Sublingual Spray Formulation of Artemether in African Children with Plasmodium falciparum Malaria. Antimicrob Agents Chemother. 2015 Nov;59(11):6930-8. doi: 10.1128/AAC.00243-15. Epub 2015 Aug 24. PubMed PMID: 26303805. 7: Sondo P, Derra K, Diallo-Nakanabo S, Tarnagda Z, Zampa O, Kazienga A, Valea I, Sorgho H, Owusu-Dabo E, Ouedraogo JB, Guiguemde TR, Tinto H. Effectiveness and safety of artemether-lumefantrine versus artesunate-amodiaquine for unsupervised treatment of uncomplicated falciparum malaria in patients of all age groups in Nanoro, Burkina Faso: a randomized open label trial. Malar J. 2015 Aug 20;14:325. doi: 10.1186/s12936-015-0843-8. PubMed PMID: 26289949; PubMed Central PMCID: PMC4545998. 8: Mekonnen SK, Medhin G, Berhe N, Clouse RM, Aseffa A. Efficacy of artemether-lumefantrine therapy for the treatment of uncomplicated Plasmodium falciparum malaria in Southwestern Ethiopia. Malar J. 2015 Aug 15;14:317. doi: 10.1186/s12936-015-0826-9. PubMed PMID: 26271736; PubMed Central PMCID: PMC4536736. 9: Pfeil J, Borrmann S, Bassat Q, Mulenga M, Talisuna A, Tozan Y. An Economic Evaluation of the Posttreatment Prophylactic Effect of Dihydroartemisinin-Piperaquine Versus Artemether-Lumefantrine for First-Line Treatment of Plasmodium falciparum Malaria Across Different Transmission Settings in Africa. Am J Trop Med Hyg. 2015 Aug 3. pii: 15-0162. [Epub ahead of print] PubMed PMID: 26240155. 10: Achieng AO, Muiruri P, Ingasia LA, Opot BH, Juma DW, Yeda R, Ngalah BS, Ogutu BR, Andagalu B, Akala HM, Kamau E. Temporal trends in prevalence of Plasmodium falciparum molecular markers selected for by artemether-lumefantrine treatment in pre-ACT and post-ACT parasites in western Kenya. Int J Parasitol Drugs Drug Resist. 2015 Jun 29;5(3):92-9. doi: 10.1016/j.ijpddr.2015.05.005. eCollection 2015 Dec. PubMed PMID: 26236581; PubMed Central PMCID: PMC4501530. 11: Wu J, Li H, Li M. Effects of artemether on the proliferation, apoptosis, and differentiation of keratinocytes: potential application for psoriasis treatment. Int J Clin Exp Med. 2015 May 15;8(5):7069-78. eCollection 2015. PubMed PMID: 26221244; PubMed Central PMCID: PMC4509189. 12: Ukah M, Badejoko O, Ogunniyi S, Loto O, Aboderin O, Fatusi A. A randomized trial of artesunate-amodiaquine versus artemether-lumefantrine for the treatment of acute uncomplicated malaria in pregnancy. Int J Gynaecol Obstet. 2015 Oct;131(1):41-4. doi: 10.1016/j.ijgo.2015.05.009. Epub 2015 Jul 3. PubMed PMID: 26169336. 13: Wasunna B, Okiro EA, Webster J, Todd J, Snow RW, Jones C. The Impact of a Community Awareness Strategy on Caregiver Treatment Seeking Behaviour and Use of Artemether-Lumefantrine for Febrile Children in Rural Kenya. PLoS One. 2015 Jul 2;10(7):e0130305. doi: 10.1371/journal.pone.0130305. eCollection 2015. PubMed PMID: 26135143; PubMed Central PMCID: PMC4489881. 14: Getnet G, Fola AA, Alemu A, Getie S, Fuehrer HP, Noedl H. Therapeutic efficacy of artemether-lumefantrine for the treatment of uncomplicated Plasmodium falciparum malaria in Enfranze, north-west Ethiopia. Malar J. 2015 Jun 24;14:258. doi: 10.1186/s12936-015-0775-3. PubMed PMID: 26105035; PubMed Central PMCID: PMC4477607. 15: Ansari MT, Hussain A, Nadeem S, Majeed H, Saeed-Ul-Hassan S, Tariq I, Mahmood Q, Khan AK, Murtaza G. Preparation and Characterization of Solid Dispersions of Artemether by Freeze-Dried Method. Biomed Res Int. 2015;2015:109563. doi: 10.1155/2015/109563. Epub 2015 May 17. PubMed PMID: 26097842; PubMed Central PMCID: PMC4449868. 16: O'Neill JF, Johnston RC, Halferty L, Hanna RE, Brennan GP, Fairweather I. A comparative study on the impact of two artemisinin derivatives, artemether and artesunate, on the female reproductive system of Fasciola hepatica. Vet Parasitol. 2015 Jul 30;211(3-4):182-94. doi: 10.1016/j.vetpar.2015.05.027. Epub 2015 Jun 6. PubMed PMID: 26093822. 17: Yalçın M, Sevim E, Duran A. [Treated with Artemether-Lumefantrine Five Evaluation of P. Falciparum Malaria Cases in Terms of Hyponatremia and Thrombocytopenia]. Turkiye Parazitol Derg. 2015 Jun;39(2):155-8. doi: 10.5152/tpd.2015.3520. Turkish. PubMed PMID: 26081891. 18: Djimde AA, Makanga M, Kuhen K, Hamed K. The emerging threat of artemisinin resistance in malaria: focus on artemether-lumefantrine. Expert Rev Anti Infect Ther. 2015 Aug;13(8):1031-45. doi: 10.1586/14787210.2015.1052793. Epub 2015 Jun 16. PubMed PMID: 26081265. 19: Denoeud-Ndam L, Dicko A, Baudin E, Guindo O, Grandesso F, Sagara I, Lasry E, Palma PP, Parra AM, Stepniewska K, Djimde AA, Barnes KI, Doumbo OK, Etard JF. A multi-center, open-label trial to compare the efficacy and pharmacokinetics of Artemether-Lumefantrine in children with severe acute malnutrition versus children without severe acute malnutrition: study protocol for the MAL-NUT study. BMC Infect Dis. 2015 Jun 12;15:228. doi: 10.1186/s12879-015-0963-3. PubMed PMID: 26068100; PubMed Central PMCID: PMC4464227. 20: Ebstie YA, Zeynudin A, Belachew T, Desalegn Z, Suleman S. Assessment of therapeutic efficacy and safety of artemether-lumefantrine (Coartem®) in the treatment of uncomplicated Plasmodium falciparum malaria patients in Bahir Dar district, Northwest Ethiopia: an observational cohort study. Malar J. 2015 Jun 5;14:236. doi: 10.1186/s12936-015-0744-x. PubMed PMID: 26045199; PubMed Central PMCID: PMC4464854.